Substituted 2-amino-3-(2-amino-phenylsulfanyl)-propionic acids

Chemistry: molecular biology and microbiology – Micro-organism – tissue cell culture or enzyme using process... – Preparing alpha or beta amino acid or substituted amino acid...

Reexamination Certificate

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C514S012200, C514S04400A, C540S491000, C560S009000

Reexamination Certificate

active

07011960

ABSTRACT:
The present invention relates to a new process for the preparation compounds of formula Iwherein R1, R2, R3and n are as described in the description which process comprises reacting compounds of formula IIwherein R1, R2, R3, n and R4are as described in the description, with a protease in an aqueous system containing an organic co-solvent.The compound of formula I are useful for the preparation of 1,5-benzothiazepines which are useful as enzyme inhibitors, such as protease, interleukin-1β-converting enzyme, elastase or angiotensin converting enzyme, GPCR antagonists (cholecystokinin, angiotensin II receptor).

REFERENCES:
patent: 6420166 (2002-07-01), Iding et al.
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patent: 407 033 (1991-01-01), None
patent: 0 560 408 (1993-09-01), None
patent: 0 577 253 (1994-01-01), None
Morton et al., Tetrahedron Letters 41, pp. 3029-3033 (2000).

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